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KN-62

Catalog #: 1277
28 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
1277/1
KN-62 | CAS No. 127191-97-3 | P2X Receptor Antagonists
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Description: Non-competitive P2X7 antagonist

Chemical Name: 4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl] phenyl isoquinolinesulfonic acid ester

Purity: ≥98%

Product Details
Citations (28)
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Biological Activity

KN-62 is a selective, cell-permeable inhibitor of CaM kinase II (IC50 = 0.9 μM). Binds directly to the calmodulin binding site of the enzyme. Potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM).

Technical Data

M.Wt:
721.84
Formula:
C38H35N5O6S2
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
127191-97-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Citations for KN-62

The citations listed below are publications that use Tocris products. Selected citations for KN-62 include:

28 Citations: Showing 1 - 10

  1. Peptide/Receptor Co-evolution Explains the Lipolytic Function of the Neuropeptide TLQP-21.
    Authors: Sahu Et al.
    Cell Rep  2019;28:2567
  2. Secreted Amyloid Precursor Protein-Alpha Promotes Arc Protein Synthesis in Hippocampal Neurons.
    Authors: Livingstone Et al.
    Front Mol Neurosci  2019;12:198
  3. Targeted Intron Retention and Excision for Rapid Gene Regulation in Response to Neuronal Activity.
    Authors: Mauger Et al.
    Neuron  2016;92:1266
  4. Neurophysiological mechanisms of bradykinin-evoked mucosal chloride secretion in guinea pig small intestine.
    Authors: Qu Et al.
    World J Gastrointest Pathophysiol  2016;7:150
  5. Endocannabinoid dynamics gate spike-timing dependent depression and potentiation.
    Authors: Cui Et al.
    Elife  2016;5:e13185
  6. Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense.
    Authors: Ledderose Et al.
    J Infect Dis  2016;213:456
  7. Identification of a new pharmacological activity of the phenylpiperazine derivative naftopidil: tubulin-binding drug.
    Authors: Ishii and Sugimura
    Cell Rep  2015;8:42618
  8. Rapid dispersion of SynGAP from synaptic spines triggers AMPA receptor insertion and spine enlargement during LTP.
    Authors: Araki Et al.
    PLoS One  2015;85:173
  9. Biophysical Regulation of Chromatin Architecture Instills a Mechanical Memory in Mesenchymal Stem Cells.
    Authors: Heo Et al.
    Sci Rep  2015;5:16895
  10. Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via iverm. induces a non-apoptotic and inflammatory form of cancer cell death.
    Authors: Draganov Et al.
    J Cell Sci  2015;5:16222
  11. Synapse-specific compartmentalization of signaling cascades for LTP induction in CA3 interneurons.
    Authors: Galván Et al.
    Neuroscience  2015;290:332
  12. Nucleotide receptors control IL-8/CXCL8 and MCP-1/CCL2 secretions as well as proliferation in human glioma cells.
    Authors: Braganhol Et al.
    Biochim Biophys Acta  2015;1852:120
  13. The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells.
    Authors: Giannuzzo Et al.
    J Chem Biol  2015;14:203
  14. Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with isoprote.
    Authors: Merino Et al.
    Sci Rep  2015;10:e0132884
  15. Heterosynaptic structural plasticity on local dendritic segments of hippocampal CA1 neurons.
    Authors: Oh Et al.
    Neuron  2015;10:162
  16. Loss of long-term depression in the insular cortex after tail amputation in adult mice.
    Authors: Liu and Zhuo
    Mol Pain  2014;10:1
  17. Role of salt-inducible kinase 1 in the activation of MEF2-dependent transcription by BDNF.
    Authors: Finsterwald Et al.
    PLoS One  2013;8:e54545
  18. OX2R activation induces PKC-mediated ERK and CREB phosphorylation.
    Authors: Guo and Feng
    Exp Cell Res  2012;318:2004
  19. Extracellular ATP exerts opposite effects on activated and regulatory CD4+ T cells via purinergic P2 receptor activation.
    Authors: Trabanelli Et al.
    J Immunol  2012;189:1303
  20. Calcium/calmodulin-dependent protein kinase II mediates group I metabotropic glutamate receptor-dependent protein synthesis and long-term depression in rat hippocampus.
    Authors: Mockett Et al.
    J Neurosci  2011;31:7380
  21. Calcium-dependent phosphorylation regulates neuronal stability and plasticity in a highly precise pacemaker nucleus.
    Authors: George Et al.
    J Neurophysiol  2011;106:319
  22. Deactivation of L-type Ca current by inhibition controls LTP at excitatory synapses in the cerebellar nuclei.
    Authors: Person and Raman
    Neuron  2010;66:550
  23. Intracellular redox state alters NMDA receptor response during aging through Ca2+/calmodulin-dependent protein kinase II.
    Authors: Bodhinathan Et al.
    J Neurosci  2010;30:1914
  24. Human eosinophils recognize endogenous danger signal crystalline uric acid and produce proinflammatory cytokines mediated by autocrine ATP.
    Authors: Kobayashi Et al.
    J Immunol  2010;184:6350
  25. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.
    Authors: Donnelly-Roberts Et al.
    Br J Pharmacol  2009;157:1203
  26. Kinase networks integrate profiles of N-MthD.-aspartate receptor-mediated gene expression in hippocampus.
    Authors: Coba Et al.
    J Biol Chem  2008;283:34101
  27. Inhibition of the ATP-gated P2X7 receptor promotes axonal growth and branching in cultured hippocampal neurons.
    Authors: Díaz-Hernández Et al.
    Mol Cancer  2008;121:3717
  28. Potentiation of TRPV3 channel function by unsaturated fatty acids.
    Authors: Hu Et al.
    J Cell Physiol  2006;208:201

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